Abstract: Compounds of formula (I) ##STR1## and salts thereof wherein R.sup.1 is a methyl, ethyl or isopropyl group;R.sup.2 is a hydrogen atom or a group OR.sup.4 (where OR.sup.4 is a hydroxyl group or a substituted hydroxyl group having up to 25 carbon atoms) and R.sup.3 is a hydrogen atom, or (when R.sup.2 is a hydrogen atom) a bromine atom; or R.sup.2 and R.sup.3 together with the carbon atom to which they are attached represent >C.dbd.CH.sub.2, >C.dbd.O or >C.dbd.NOR.sup.5 (where R.sup.5 is a hydrogen atom, a C.sub.1-8 alkyl group or a C.sub.3-8 alkenyl group and the group >C.dbd.NOR.sup.5 is in the E configuration); andY represents an oxygen atom or a group NOR.sup.5 (where R.sup.5 is as defined above); with the proviso that when Y is an oxygen atom and R.sup.1 is an isopropyl group, then R.sup.2 is other than hydroxyl group.These compounds may be used for controlling insect, acarine, nematode or other pests.

Abstract: This invention relates to the field of immune therapy of cancer, more specifically to immunoconjugates of a cytotoxic moiety with a targeting moiety, more specifically to immunoconjugates of antibodies or fragments or functional derivatives of antibodies coupled to a cytotoxic substance such as drugs, toxins or radioisotopes. It especially relates to the release of substances bound to a targeting moiety through the use of acid-cleavable linker molecules.

Abstract: There is disclosed a series of macrolides isolated from the fermentation broth of microorganisms identified as MA-6825, MA-6864 and MA-6865. The structure of the novel compounds isolated from the microorganisms is presented based upon analytical studies. The compounds are highly potent antiparasitic, insecticidal, and anthelmintic agents and are related to the class of macrolides known as milbemycins. Compositions for such uses are also disclosed.

Abstract: Avermectin compounds are substituted at the 4a-position: the 4a-methyl group is first derivatized with a hydroxy group which is then substituted with a variety of alkyl, alkoxy alkyl, or polyalkoxy alkyl groups and derivatives thereof. The compounds are potent antiparasitic and anthelmintic agents and compositions for such uses are also disclosed.

Abstract: Avermectin analogs are prepared where the 23-position ring carbon atom is deleted and replaced by an oxygen atom. The compounds are prepared by opening the outer spiroketal ring to gain access to the 23-position atom, substituting the ring-opened compounds with a substituent containing the oxygen atom in the appropriate position and closing the ring to prepare the desired compounds. The compounds are potent anthelmintic agents and methods and compositions including such 23-nor-23-oxa compounds are also disclosed.

Abstract: There are disclosed avermectin derivatives which are avermectin modified at the 3- and 4-positions. The 3-hydroxy and 4-keto, epoxide and hydroxy (hydroxymethyl) derivatives and the 4-oxo compound are prepared from the natural avermectin by moving the 3,4-double bond exocyclic at 4 and forming a 3-hydroxy group. Osmolation gave an .alpha.,.beta.-diol across the double bond and cleavage of the diol provided the 4-oxo compound. The 4-oxo compound is epoxidized with an ylide reagent. The compounds are useful as anthelmintic agents and compositions for that use using the compounds as the active ingredient thereof are also described.

Abstract: The natural stereochemistry at the 13-position of avermectin aglycones, normally .alpha.-oriented or below the plane of the molecule, is inverted or epimerized into the .beta.-position. The procedure starts with the avermectin aglycone compounds where the 13.alpha.-hydroxy group is activated to a mesylate leaving group. The resultant 13-.alpha.-mesylate is then displaced with a cesium carboxylate and one equivalent of the respective carboxylic acid, ending with the ester group being converted to the 13-.beta.-hydroxy configuration by transesterification in high yield.

Abstract: A novel antibiotic complex, A59770, individual factors and derivatives thereof, are provided. The A59770 compounds are useful as pesticides, particularly as rodenticides. Further provided are methods for reducing a rodent population, rodenticidal compositions, and an A59770-producing Amycolatopsis orientalis culture.

Abstract: Avermectin derivatives are disclosed which incorporate two fluorine atoms at the 4' monosaccharide position, the 4" disaccharide position or the 23 position. Avermectin aglycone derivatives are also disclosed which incorporate two fluorine atoms at position 13 or 23. These difluoro avermectin analogs are derived from corresponding ketones and enones which in turn are prepared by chemical modification of naturally occurring avermectins. These compounds are used as antiparisitic, insecticidal and antihelmintic agents in humans and animals and compositions containing such compounds as the active ingredient thereof are also disclosed.

Abstract: Avermectin compounds are substituted at the 4", 4' or 13-postion hydroxy group with an alkylthioalkyl group and are optionally substituted at the other reactive positions of the avermectin molecule. The compounds are prepared by reacting protected avermectins, avermectin monosaccharides or avermectin aglycones with dialkylsulfoxides. The compounds are potent antiparasitic agents and compositions for such uses are also disclosed.

Abstract: 13-Hydroxy-5-ketomilbemycin derivatives are prepared by oxidizing a 5-ketomilbemycin with selenium dioxide in the presence of a lower aliphatic carboxylic acid. A range of new 13-acyloxy-5-ketomilbemycins and a method of preparing them are also disclosed.

Abstract: Compounds of formula (I) ##STR1## and salts thereof, wherein R.sup.1 represents a methyl, ethyl or ispropyl group; R.sup.2 represents a C.sub.2-7 alkyl group interrupted by an oxygen or sulphur atom or an aryl, aryl C.sub.1-7 alkyl or heteroaryl C.sub.1-7 alkyl group; OR.sup.3 is a hydroxyl group or a substituted hydroxyl group having up to 25 carbon atoms; and the group .dbd.NOR.sup.2 is in the E configuration.These compounds may be used for controlling insect, acarine, nematode or other pests.

Abstract: Avermectin analogs are disclosed wherein the 6,6-spiroketal ring system has been reduced in size to a 6,5-spiroketal ring system by the deletion of the 25-position carbon atom and the 25-alkyl substituent. This is accomplished by opening the outer spiroketal ring with the elimination of ring carbon atoms 23, 24 and 25 and the alkyl substituent at the 25-position and incorporation a new component, reclosing the spiroketal to a 5-membered ring with new substituents at the 24-position. The compounds are used as anti-parasitic insecticidal and anti-helmintic agents in humans and animals and compositions containing such compounds as the active ingredient thereof are also disclosed.

Abstract: Avermectin analogs are disclosed wherein the 6,6-spiroketal ring system has been reduced in size to a 6,5-spiroketal ring system by the deletion of the 25-position carbon atom and the 25-alkyl substituent and which has a 23-acyl cycloalkyl, phenyl or substituted hydroxymethyl substituent. This is accomplished by opening the outer spiroketal ring with the elimination of ring carbon atoms 23, 24 and 25 and the alkyl substituent at the 25-position and incorporation a new component, reclosing the spiroketal to a 5-membered ring with a 23-acyl substituent and new substituents at the 24-position. The compounds are used as anti-parasitic insecticidal and anti-helmintic agents in humans and animals and compositions containing such compounds as the active ingredient thereof are also disclosed.

Abstract: This invention relates to new agents designated LL-F28249.alpha., LL-F28249.beta., LL-F28249.gamma., LL-F28249.delta., LL-F28249.epsilon., LL-F28249.zeta., LL-F28249.eta., LL-F28249.theta., LL-F28249.iota., LL-F28249.kappa., LL-F28249.lambda., LL-F28249.mu., LL-F28249.nu., and LL-F2924.omega., to their production by fermentation, to methods for their recovery and concentration from crude solutions, to processes for their purification and to pharmaceutically and pharmacologically-acceptable salts thereof. The present invention includes within its scope the biologically pure culture which produces there agents, derived from a newly-discovered and previously uncultured microorganism, Streptomyces cyaneogriseus subsp. noncyanogenus, NRRL 15773.

Abstract: Bisphthalide lactones of formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3 and R.sub.4 are each independently of one another hydrogen, alkyl of at most 12 carbon atoms which is unsubstituted or substituted by halogen, hydroxy, cyano, tetrahydrofuryl or lower alkoxy; or are acyl of 1 to 12 carbon atoms, cycloalkyl of 5 to 10 carbon atoms or unsubstituted aralkyl or aryl, or aralkyl or aryl each substituted by halogen, cyano, nitro, trifluormethyl, lower alkyl, lower alkoxy, lower alkoxycarbonyl, --NX'X"-- or 4--NX'X--"phenylamino, wherein X' and X" are each independently of the other hydrogen, lower alkyl, cyclohexyl, benzyl or phenyl, or the pairs of substituents --NR.sub.1 R.sub.2 and --NR.sub.3 R.sub.4 are each a 5- or 6-membered, preferably saturated, heterocyclic radical, V.sub.1 and V.sub.2 are hydrogen, halogen, lower alkyl, C.sub.1 -C.sub.12 alkoxy, C.sub.1 -C.sub.

Abstract: The present invention relates to novel 5-acyl, 23-acyl and 5,23-diacyl derivtaives of the LL-F28249 compounds. These LL-F28249 compounds (collectively) are isolates from the fermentation broth of Streptomyces cyaneogriseus subspecies noncyanogenus having deposit accession number NRRL 15773. The present 5-acyl and 5,23-diacyl compounds are prepared by selective acylation using acid chlorides or anhydrides in the presence of 4-dimethylaminopyridine. The 23-acyl compounds are prepared by selective acylation of the 5-O-silylated LL-F28249 compounds. These novel compounds have potent anthelmintic, insecticidal, ectoparasiticidal, nematicidal and acaricidal activity. Compositions containing these derivatives of LL-F28249 also are described herein.

Abstract: Fermentation of S. erythraea produces the novel avermectin, 28-hydroxy ivermectin aglycone.

Abstract: The present invention relates to novel derivatives of formula I that can be derived from milbemycins, to their preparation and their use for controlling pests, and also to pesticides that contain at least one of these compounds as active ingredient.The novel compounds have the general formula I ##STR1## in which X is one of the groups --CH(OR.sub.1)--, --C(O)-- or --C(.dbd.N--OR)--;R.sub.1 is hydrogen or an OH-protecting group;R is hydrogen, an OH-protecting group, or an alkyl or cycloalkyl group;R.sub.2 is methyl, ethyl, isopropyl or sec.-butyl; andPh is a phenyl ring that is substituted by R.sub.a, R.sub.b, R.sub.c and R.sub.d, wherein each of R.sub.a, R.sub.b, R.sub.c and R.sub.d, independently of the others, is hydrogen, C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkoxyalkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.1 -C.sub.10 alkoxy, C.sub.2 -C.sub.10 alkoxyalkoxy, or a phenyl or phenoxy radical that is unsubstituted or is substituted by at least one substituent from the group C.sub.1 -C.sub.3 alkyl and C.sub.

Abstract: Water soluble salts of purpuromycin, their use for the topical treatment of infectious vaginitis and topical dosage forms containing said products. Oral and parenteral formulations for administration of the water soluble purpuromycin salts. The water soluble salts of purpuromycin are simultaneously active against the main causative agents of infectious vaginitis i.e.: Candida vaginalis, Trichomonas vaginalis and Gardnerella vaginalis.

Abstract: Compounds of formula (1) ##STR1## wherein R represents a sugar residue or an acylated derivative thereof;R.sup.1 represents a methyl, ethyl or isopropyl group;Y.sup.1 is --CH.sub.2, Y.sup.2 is --CH-- and X represents ##STR2## [wherein R.sup.2 represents a hydrogen atom or a group OR.sup.6 (where OR.sup.6 is a hydroxyl group or a substituted hydroxyl group having up to 25 carbon atoms) and R.sup.3 represents a hydrogen atom, or R.sup.2 and R.sup.3 together with the carbon atom to which they are attached represent >C.dbd.0, >C.dbd.CH.sub.2 or >C.dbd.NOR.sup.7 (where R.sup.7 represents a hydrogen atom, a C.sub.1-8 alkyl group or a C.sub.3-8 alkenyl group) and the group >C.dbd.NOR.sup.7 is in the E configuration] or --Y.sup.1 --X--Y.sup.2 -- represents --CH.dbd.CH--CH-- or --CH.sub.2 --CH.dbd.C--; andR.sup.4 represents a group OR.sup.6 as defined above and R.sup.5 represents a hydrogen atom, or R.sup.4 and R.sup.5 together with the carbon atom to which the are attached represent >C.dbd.0 or >C.

Abstract: Compounds of formula (1) ##STR1## wherein R.sup.1 represents a methyl, ethyl or isopropyl group; Y.sup.1 is --CH.sub.2 --, Y.sup.2 is --CH-- and X represents ##STR2## [where R.sup.2 represents a hydrogen atom or a group OR.sup.6 (where OR.sup.6 is a hydroxy group or a substituted hydroxyl group having up to 25 carbon atoms) and R.sup.3 represents a hydrogen atom, or R.sup.2 and R.sup.3 together with the carbon atom to which they are attached represent >C.dbd.O, >C.dbd.CH.sub.2 or >C.dbd.NOR.sup.7 (where R.sup.7 represents a hydrogen atom, a C.sub.1-8 alkyl group or a C.sub.3-8 alkenyl group and the group >C.dbd.NOR.sup.7 is in the E configuration)] or --Y.sup.1 --X--Y.sup.2 represents --CH.dbd.CH--CH-- or --CH.sub.2 --CH.dbd.C--; R.sup.4 represents a group OR.sup.6 as defined above and R.sup.5 represents a hydrogen atom, or R.sup.4 and R.sup.5 together with the carbon atom to which they are attached represent >C.dbd.O or >C.dbd.NOR.sup.7a ( where R.sup.7a is as defined above for R.sup.

Abstract: Compounds of formula (1) ##STR1## and their salts, wherein R.sup.1 is a methyl, ethyl or isopropyl group each substituted by a hydroxyl group or R.sup.1 is a group --(CH.sub.2).sub.n R7 or a group --CH(CH.sub.3)R.sup.7 (where n is zero or 1 and R.sup.7 l is CHO or CO.sub.2 H);Y.sup.1 is --CH.sub.2 --, Y.sup.2 is --CH-- and X represents ##STR2## [where R.sup.2 is a hydrogen atom or a group OR.sup.8 is a hydroxyl group or a substituted hydroxyl group having up to 25 carbon atoms) and R.sup.3 is a hydrogen atom, or R.sup.2 and R.sup.3 together with the carbon atom to which they are attached represent >.dbd.O, >C.dbd.CH.sub.2 or >C.dbd.NOR.sup.9 (where R.sup.9 is a hydrogen atom or a C.sub.1-8 alkyl or C.sub.3-8 alkenyl group) and the group >C.dbd.NOR.sup.9 is in the E configuration] or --Y.sup.1 --X--Y.sup.2 -- represents --CH.dbd.CH--CH-- or --CH.sub.2 --CH.dbd.C--;R.sup.4 is a group OR.sup.8 as defined above and R.sup.5 is a hydrogen atom, or R.sup.4 and R.sup.

Abstract: This invention relates to new agents designated LL-F28249.alpha., LL-F28249.beta., LL-F28249.gamma., LL-F28249.delta., LLF28249.epsilon., LL-F28249.zeta., LL-F28249.eta., LL-F28249.theta., LL-F28249.iota., LL-F28249.kappa., LL-F28249.lambda., LL-F28249.mu., LL-F28249.nu., and LL-F28249.omega., to their production by fermentation, to methods for their recovery and concentration from crude solutions, to processes for their purification and to pharmaceutically and pharmacologically-acceptable salts thereof. The present invention includes within its scope the biologically pure culture which produces there agents, derived from a newly-discovered and previously uncultured microorganism, Streptomyces cyaneogriseus subsp. noncyanogenus, NRRL 15773.

Abstract: Compounds of formula (I) ##STR1## and salts thereof, wherein R is a C.sub.1-4 alkyl group, R.sup.1 is a methyl, ethyl or isopropyl group; and OR.sup.2 is a hydroxyl or substituted hydroxyl group having up to 25 carbon atoms.These compounds may be used for controlling insect, acarine, nematode or other pests.

Abstract: Novel HMG-CoA reductase inhibitors are useful as antihypercholesterolemic agents and are represented by structural formulae (I) and (II): ##STR1##

Abstract: The invention provides novel compounds having the formula: ##STR1## wherein R when taken individually is H; R.sup.1 when taken individually is H or OH; R and R.sup.1 when taken together represent a double bond;R.sup.2 is an alpha-branched C.sub.3 -C.sub.8 alkyl, alkenyl, alkynyl, alkoxyalkyl or alkylthioalkyl group; a C.sub.3 -C.sub.8 cycloalkyl, C.sub.5 -C.sub.8 cycloalkenyl or C.sub.5 -C.sub.8 cycloalkylalkyl group, any of which may be substituted by methylene or one or more C.sub.1 -C.sub.4 alkyl groups or halo atoms; or a 3 to 6 membered oxygen or sulphur containing heterocyclic ring which may be substituted by one or more C.sub.1 -C.sub.4 alkyl groups or halo atoms;R.sup.3 is hydrogen or methyl;R.sup.4 is H or 4'-(alpha-L-oleandrosyl)-alpha-L-oleandrosyloxy with the proviso that when R.sup.2 is alkyl it is not isopropyl or sec-butyl; when R.sup.4 is H, each of R and R.sup.1 is H, and R.sup.2 is not methyl or ethyl; and when R.sup.4 is H, R is H, R.sup.1 is OH, and R.sup.

Abstract: There are disclosed avermectin aglycone derivatives which incorporate a ketal at position 13. The synthetic ketal analogs are derived from the corresponding ketones which in turn are prepared by chemical modification of naturally occurring avermectins. The compounds are active antiparasitic agents and compositions for that use are disclosed.

Abstract: An antibiotic compound of the formula: ##STR1## is an antiparasitic agent active against insect pests, acari, free living nematodes and endo- and ectoparasites. It is prepared by fermentation using the microorganism Streptomyces griseochromogenes ATCC 53928.

Abstract: New benz[b]pyranes and pyranopyridines of formula I, ##STR1## wherein the significances of substituents V, T, W, R.sub.3 to R.sub.5, R.sub.9, R.sub.10, m, X, Y and Z are given in claim 1 and their N-oxides and their salts and their use in the treatment of raised blood pressure in the treatment of vascular disorders and other disorders in which a reduction in tension of the smooth muscles is therapeutically useful, as well as in the treatment of hair loss and baldness. Further the compounds are useful in the treatment of asthma and obstructive disorders of the respiratory system as well as in the prophylactic treatment of obstructive or inflammatory airways disease, for example asthma, as well as novel pharmaceutical compositions comprising said K.sup.+ channel activators suitable for such use.

Abstract: Compounds of formula (I): ##STR1## wherein R.sup.1 is methoxy or optionally protected hydroxy have anthelmintic activity and are useful in the treatment of helminthiasis in humans and animals.

Abstract: There are disclosed novel avermectin derivatives wherein the outer oleandrose ring of avermectin or avermectin monosaccharide is homologated by addition of diazomethane to 4"- or 4'-oxo-avermectin to afford the perhydrooxepine derivatives. The homologated avermectins can then be further derivatized to afford additional novel avermectins. The new compounds are potent antiparasitic agents, in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.

Abstract: Compounds of formula (1) ##STR1## and salts thereof, wherein R.sup.1 represents a methyl, ethyl or isopropyl group;Y.sup.1 is --CH.sub.2 --, Y.sup.2 is --CH-- and X represents ##STR2## where R.sup.2 represents a hydrogen atom or a group OR.sup.8 (where OR.sup.8 is a hydroxyl group or a substituted hydroxyl group having up to 25 carbon atoms) and R.sup.3 represents a hydrogen atom, or R.sup.2 and R.sup.3 together with the carbon atom to which they are attached represent >C.dbd.O, >C.dbd.CH.sub.2 or >C.dbd.NOR.sup.9 (where R.sup.9 represents a hydrogen atom, a C.sub.1-8 alkyl group or a C.sub.3-8 alkenyl group) and the group >C.dbd.NOR.sup.9 is in the E configuration] or --Y.sup.1 --X--Y.sup.2 -- represents --CH.dbd.CH--CH-- or --CH.sub.2 --CH.dbd.C--;R.sup.4 represents a group OR.sup.8 as defined above and R.sup.5 represents a hydrogen atom, or R.sup.4 and R.sup.5 together with the carbon atom to which they are attached represent >C.dbd.O or >C.dbd.NOR.sup.9a (where R.sup.

Abstract: There are disclosed avermectin derivatives in which position 13 of the avermectins has been inverted from the normal (alpha) stereoschemistry to the epimeric 13-beta stereochemistry. The synthetic 13-epi analogs are derived from the corresponding aglycones which in turn are prepared by chemical modification of naturally occurring avermectins. The compounds are active antiparasitic agents and compositions for that use are disclosed.

Abstract: There are provided certain 13-alkyl-23-imino-LL-F28249 compounds which are useful for controlling endo- and ectoparasites, insects, acarids and nematodes.

Abstract: Compounds of formula (I): ##STR1## wherein R.sup.1 is hydrogen or optionally protected hydroxy; R.sup.2 is alkoxy, optionally protected hydroxy, oxo or optionally O-substituted oximino; R.sup.3 is hydrogen, optionally protected hydroxy, or a group 4'-(.alpha.-L-oleandrosyl)-.alpha.-L-oleandrosyloxy or .alpha.-L-oleandrosyloxy wherein the terminal hydroxy group is optionally protected; one or R.sup.4 and R.sup.5 is hydrogen and the other is methyl; and one of R.sup.6 and R.sup.7 is hydrogen and the other is methyl; with the proviso that (a) when R.sup.1 is optionally protected hydroxy, R.sup.3 is hydrogen, and (b) when R.sup.2 is not methoxy or optionally protected hydroxy, R.sup.1 and R.sup.3 are both hydrogen, are new and useful as anthelmintic agents.

Abstract: A process for the preparation of a compound of formula (I) ##STR1## (in which R.sup.1 is methyl, ethyl or isopropyl) by hydrogenation of a corresponding compound having a double bond at the 22,23-position, for example in the presence of a rhodium catalyst.

Abstract: There are provided certain 13-halo-23-imino-LL-F28249 compounds which are useful for controlling endo- and ectoparasites, insects, acarids and nematodes.

Abstract: A process for preparing a compound of formula (I) ##STR1## (where (i) R.sup.1 is an ethoxy group and R.sup.2 is a hydrogen atom, (ii) R.sup.1 is a hydrogen atom and R.sup.2 is a bromine atom or (iii) (R.sup.1 and R.sup.2 together with the carbon atom to which they are attached represent>C.dbd.O) which comprises stereoselectively reducing the corresponding 5-keto compound.

Abstract: The present invention relates to novel derivatives of LL-F28249 compounds wherein the 23-hydroxy group is eliminated to introduce a double bond at the 23,24 position. These resulting derivatives are .DELTA..sup.23 -LL-F28249 compounds. These LL-F28249 precursor compounds preferably are derived via a controlled microbiological fermentation of Streptomyces cyaneogriseus subsp. noncyanogenus having deposit accession number NRRL 15773. The novel derivatives of the present invention possess activity as anthelmintic, ectoparasitic, insecticidal, acaricidal and nematicidal agents. They also are useful in areas of human and animal health and in agricultural crops.

Abstract: Novel avermectin derivatives are disclosed, wherein the 5-hydroxy group is replaced by an oxime group. The avermectin-5-oximes can further be derivatized at the 4"- or 4'-positions as amino, substituted amino, acylhydrazone, semicarbazone, or substituted semicarbazone analogues. The avermectin-5-oximes are prepared by the oxidation of the 5-hydroxy compounds with manganese dioxide or with pyridinium dichromate to the known 5-oxo analogues, and these are then reacted with a hydroxylamine salt. The new compounds are potent anti-parasitic agents, in particular, the compounds are anthelmintic, insecticidal and acaricidal agents.

Abstract: There are disclosed new compounds with significant antiparasitic activity which are prepared by fermenting compounds identified as LL-F28249 in a novel microorganism identified as Streptomyces avermitilis MA-5542. The LL-F28249 compounds are modified by the microorganism by hydroxylation of the 25-position terminal methyl group. The compounds are significant antiparasitic and anthelmintic agents and compositions for that use are also disclosed.

Abstract: Compounds with acaricidal, insecticidal and anthelmintic activities have the formula: ##STR1## wherein: --X--Y-- is selected from the group consisting of --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --CHOH--, --CH.dbd.CH--, and --CH.sub.2 --C(.dbd.O)--;R.sup.1 is selected from the group consisting of a methyl group, an ethyl group, an isopropyl group, a sec-butyl group and groups of formula --C(CH.sub.3).dbd.CHR.sup.5 in which R.sup.5 is selected from the group consisting of a methyl group, an ethyl group and an isopropyl group;R.sup.2 represents a group of formula --(CH.sub.2).sub.n --C(R.sup.6).dbd.C(R.sup.7)(R.sup.8) in which n is 0, 1 or 2, R.sup.6 and R.sup.7 each is selected from the group consisting of a hydrogen atom and a methyl group and R.sup.8 is selected from the group consisting of a hydrogen atom, a C.sub.1-4 alkyl group, a phenyl group and a phenyl group substituted with at least one substituent selected from the group consisting of halogen, methyl and nitro substitutents;R.sup.

Abstract: There are disclosed novel avermectin compounds having a cleaved furan ring and a hydroxy group in the 8a position. Processes for preparing these novel compounds are also disclosed. These compounds have utility as anti-parasitic agents and as insecticides against agricultural pests.

Abstract: There is disclosed an improved process for substitution of the hydroxy group at 2-position of an ascorbic acid derivative according to the following reaction scheme: ##STR1## wherein R.sup.0 is hydrogen, alkyl having 1 to 6 carbon atoms, phenyl or a group of the formula ##STR2## (wherein X is two hydrogen atoms, or acetal or ketal residue); R.sup.1 is an alkyl or alkenyl group having up to 22 carbon atoms which may be substituted with phenyl or alkoxy having 1 to 22 carbon atoms; Y is halogen or optionally substituted sulfonyloxy; R is hydrogen, or primary, secondary or tertiary alkyl having 1 to 10 carbon atoms; and Z is an alkali metal or an alkali earth metal. There is also disclosed hydrolysis of the following scheme: ##STR3## wherein R.sup.1 is as defined above; and X is acetal or ketal residue.

Abstract: Disclosed are novel 3-hydroxy-3-methylglutarylcoenzyme A reductase inhibitors useful as antihypercholesterolemic agents represented by the formula ##STR1## and the corresponding ring-opened hydroxy acids and esters derived therefrom and pharmaceutically acceptable salts thereof.Pharmaceutical compositions containing said compounds and method of inhibiting the biosynthesis of cholesterol therewith are also disclosed.

Abstract: Disclosed are novel 3-hydroxy-3-methylglutaryl-coenzyme A reductase inhibitors useful as antihypercholesterolemic agents represented by the formula ##STR1## and the corresponding ring-opened hydroxy acids derived therefrom and pharmaceutically acceptable salts thereof.Phamaceutical compositions containing said compounds and method of inhibiting the biosynthesis of cholesterol therewith are also disclosed.

Abstract: Compounds are described of formula (1) ##STR1## and salts thereof wherein R.sup.1 is a methyl, ethyl or isopropyl group;R.sup.2 represents a hydrogen atom or a group OR.sup.4 (where OR.sup.4 is a hydroxyl group or a substituted hydroxyl group having up to 25 carbon atoms) and R.sup.3 represents a hydrogen atom, or R.sup.2 and R.sup.3 together with the carbon atom to which they are attached represent >C.dbd.CH.sub.2, >C.dbd.O or >C.dbd.NOR.sup.5 (where R.sup.5 is a hydrogen atom or a C.sub.1-8 alkyl group and the group >C.dbd.NOR.sup.5 is in the E configuration).These compounds may be used for controlling insect, acarine, nematode or other pests.

Abstract: Compounds of the formula ##STR1## the use thereof for inhibiting cholesterol biosynthesis and lowering the blood cholesterol level and, therefore, in the treatment of hyperlipoproteinemia and atherosclerosis, pharmaceutical compositions comprising such compounds and processes for and intermediates in the synthesis of such compounds.

Abstract: Compounds are described of formula (I) ##STR1## and salts therof, wherein R.sup.1 represents a methyl, ethyl or isopropyl group;R.sup.2 is alkyl; alkyl substituted by a carboxy or alkoxycarbonyl; alkenyl; phenyl or phenalkyl;R.sup.3 is --OH;OR.sup.4 is a hydroxyl group or a substituted hydroxyl group having up to 25 carbon atoms.These compounds may be used for controlling insect, acarine, nematode or other pests.